Learning objectives
The aim of the course is to provide the students with the thermodynamic concepts necessary to the knowledge and the understanding of the interconversion of the energy in biological systems (bioenergetics) as well the ligand-biomacromolecule interactions. The molecular basis of protein-ligand complex ormation will be provided together with the biochemical basis of drug action.
Learning results
At the end of the course, the student will have acquired extensive knowledge and deep understanding of the interactions between ligands and biological macromolecules. Such knowledge will be applied to the interpretation of the molecular mechanisms of drug action.
Prerequisites
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Course unit content
Modul of Biological Physical Chemistry (6 CFU) Prof. C. Compari
-Thermodynamics and Biochemistry.
- Changes of state: physical transformations of pure substances.
- Macromolecules in solution.
- Chemical equilibria involving macromolecules.
- Bioenergetics.
- Intermolecular forces.
- Colloid Chemistry.
- Non-viral vectors for gene therapy.
Pharmaceutical Biochemistry (6 CFU) Prof. B. Campanini
- Definition of drug and drug target.
- Binding properties of proteins.
- Enzymes as drug target.
- Treatment of HIV and NSAIDs as examples of the therapeutic use of enzyme inhibitors.
- Receptors as drug targets.
- Recombinant drugs.
Full programme
Modul of Biological Physical Chemistry (6 CFU) Prof. C. Compari
-Thermodynamics and Biochemistry: heat, work and energy. First law of thermodynamics. Molecular interpretation of thermodynamic quantities. Entropy, free energy and equilibrium. Second law of thermodynamics. Experimental Thermochemistry. Calorimetry. An outline of Statistical Thermodynamics.
- Changes of state: physical transformations of pure substances. Phase diagrams. Gibbs phase rule.
- Macromolecules in solution: thermodynamics and equilibria. Partial molar quantities, the chemical potential, ideal and non-ideal solutions. Application of the chemical potential to membrane equilibria: membrane equilibria, dialysis equilibrium, osmotic pressure, membrane potential.
- Chemical equilibria involving macromolecules: chemical equilibrium, thermodynamics of chemical reactions in solution. Interaction between macromolecules, binding equilibria, binding curves, cooperativity.
- Bioenergetics: molecules through membranes: transport modes, endoergonic and exoergonic reaction, coupled reactions.
- Intermolecular forces: van der Waals forces, hydrogen bond, hydrophobic interactions.
- Colloid Chemistry: definition and classification, surface tension, DLVO theory, structure and classification of surfactants, micelle and liposome.
- Non-viral vectors for gene therapy: non-viral methods for gene transfection. New non-viral vectors for gene therapy: cationic surfactants
Pharmaceutical Biochemistry (6 CFU) Prof. B. Campanini
• Drug and drug target: definition
• Binding properties of proteins
• Enzymatic catalysis
• Intracellular receptors
• GPCRs
• Receptor tyrosine kinases
• Tyr kinase-associated receptors
• Receptor guanylyl cyclases
• Enzyme inhibition and rug discovery:
o Enzymes as drug targets
o Reversible inhibitors
o Irreversible inhibitors
o Tight-binding and slow-binding inhibitors
o NSAIDs
o Enzyme inhibition in HIV therapy
• Transporters
• Overview of recombinant drugs
Bibliography
Modul of Biological Physical Chemistry (6 CFU) Prof. C. Compari
- K.E. Van Holde, W. C. Johnson, P.S. Ho Principles of Physical Biochemistry, Pearson Prentice Hall
- P. Atkins, J. De Paula, Chimica Fisica Biologica 1, Zanichelli, Bologna
- P. Atkins, J. De Paula, Elememti di Chimica Fisica, Zanichelli, Bologna
- P. Atkins, J. De Paula, Chimica Fisica, Zanichelli, Bologna.
- David G. Nicholls Bioenergetics Academic press, inc.
- Scientific reviews on specific topics
Pharmaceutical Biochemistry (6 CFU) Prof. B. Campanini
- Selected scientific papers and copy of slides can be downloaded from the Elly website.
- David L. Nelson, Michael M. Cox
- I PRINCIPI DI BIOCHIMICA DI LEHNINGER 5 ed, ZANICHELLI.
- Copeland R. Evaluation of enzyme inhibition in drug discovery, Wiley.
Teaching methods
Modul of Biological Physical Chemistry (6 CFU) Prof. C. Compari
- During the oral lesson will present the basic concepts of physical chemistry with particular emphasis on biological applications is also planned a visit to the laboratories of Physical Chemistry of the Department of Pharmacy in order to show students the techniques that have been discussed.
Modul of Pharmaceutical Biochemistry (6 CFU) Prof. B. Campanini
- Oral lessons integrated with informatic tools and the support of multimedia
Assessment methods and criteria
The final mark of the examination will be the mean of the marks obtained in the individual modules.
Modul of Biological Physical Chemistry (5 CFU) Prof. C. Compari
During the course, two written in itinere tests will be proposed. The mark of the module will be the mean of the two tests.
Alternatively, an oral examination will have to be passed, during normal examination sessions of module of pharmaceutical biochemistry.
In every case, written and oral open questions will have the purpose of establishing the level of knowledge and understanding of the course content, in relation to the educational goals.
If the results of the test will be positive (18/30), the final mark of drug-biomolecules interaction examination will be the mean of the mark of the two modules.
Modul of Pharmaceutical Biochemistry (6 CFU) Prof. B. Campanini
The exam is either a written "in itinere" test or a final oral exam.
The written test will take place during the teaching semester and will consist of two tests, dealing with the first and second part of the programm, respectively. The teaching module final mark is the average of the marks of the two tests.
During the exam period the students can take the oral exam together with the Biological Physical Chemistry module.
Other information
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